THEMED ISSUE: GPCR RESEARCH PAPER Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology

2009 
receptors are unknown; this was examined using the recombinant receptor and Biomolecular Interaction Detectiontechnology. Mouse isolated colon was mounted in tissue baths for isometric recording of neuronal contractions evoked byelectrical field stimulation (EFS), or under an intraluminal pressure gradient to induce peristalsis; the effects of RS-127445 onEFS-induced and on peristaltic contractions were measured. Faecal output of rats in grid-bottom cages was measured over 3 hfollowing i.p. RS-127445 and separately, validation of the effective doses was achieved by determining the free, unboundfraction of RS-127445 in blood and brain.Key results: RS-127445 (up to 1 mmol·L
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